Art. -Nr.: HY-18637

LDN-57444

20 Cited Publications

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Based on 20 publication(s) in Google Scholar

LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC₅₀ of 0.88 μM and a K_i of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC₅₀ of 25 μM.

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Reinheit: 99.21%
CAS. Nr.: 668467-91-2
Formel: C₁₇H₁₁Cl₃N₂O₃
Molecular Weight:397.64

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

LDN-57444 Chemical Structure

CAS. Nr.: 668467-91-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (20)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 0.88 μM (UCH-L1), 25 μM (UCH-L3)^[1]
Ki: 0.40 μM (UCH-L1)^[1]

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen :

In Vitro

LDN-57444 is a reversible, competitive inhibitor of UCH-L1, with an IC₅₀ of 0.88 μM, and also suppresses UCH-L3 activity, with an IC₅₀ of 25 μM^[1]. LDN-57444 (LDN, 5 μM for 1 hr) inhibits 70% of Uch activity in hippocampal slices of the mouse brain. LDN-57444 (5 μM for 2 hr) does not reduce potentiation further in APP/PS1 slices or in wt slices exposed to 200 nM Aβ^[2]. LDN-57444 (25-100 μM) inhibits ubiquitin-proteasome activity dose-dependently in SK-N-SH cells. LDN-57444 (50 μM) also induces apoptotic cell death, causes the endoplasmic reticulum stress and results in expression of spliced XBP-1(XBP-1s, 48KD) in SK-N-SH cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

LDN-57444 (0.4 mg/kg, i.p.) blocks the beneficial effect of V-Uch-L1, and worsens contextual conditioning performance as the mice are exposed to the context at 1, 7, 14, and 21 days after training^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 668467-91-2
Appearance Solid
Molecular Weight 397.64
Formel C₁₇H₁₁Cl₃N₂O₃
Color Light yellow to yellow
SMILES

O=C1N(CC2=CC(Cl)=CC=C2Cl)C3=C(C=C(Cl)C=C3)/C1=N/OC(C)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (20)

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Journal Impact Factor

Nat Commun

USP2 inhibition unleashes CD47-restrained phagocytosis and enhances anti-tumor immunity. [Abstract]

2025 May 16;16(1):4564. PMID: 40379682
Nat Commun

USP8 inhibition reshapes an inflamed tumor microenvironment that potentiates the immunotherapy. [Abstract]

2022 Mar 31;13(1):1700. PMID: 35361799
Redox Biol

USP20 governs tyrosine kinase inhibitors resistance through ferroptosis evasion by targeting GPX4 in cancers. [Abstract]

2026 May:92:104086. PMID: 41844497
J Immunother Cancer

CD47 destabilization via manipulating the SPOP-USP2 axis augments macrophage phagocytosis and cancer immunotherapy. [Abstract]

2026 Jan 14;14(1):e013498. PMID: 41534899
Cell Chem Biol

Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2. [Abstract]

2021 Jun 17;28(6):855-865.e9. PMID: 33979649
EMBO J

USP8 promotes cancer progression and extracellular vesicle-mediated CD8+ T cell exhaustion by deubiquitinating the TGF-β receptor TβRII. [Abstract]

2022 Aug 16;41(16):e108791. PMID: 35811497
J Med Chem

Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer. [Abstract]

2022 Oct 27;65(20):13645-13659. PMID: 36221183
Hypertens Res

Inhibition of UCHL1 by LDN-57444 attenuates Ang II-Induced atrial fibrillation in mice. [Abstract]

2020 Mar;43(3):168-177. PMID: 31700166
Cancer Sci

Ubiquitin C-terminal hydrolase L1 promotes expression of programmed cell death-ligand 1 in non-small-cell lung cancer cells. [Abstract]

2020 Sep;111(9):3174-3183. PMID: 32539182
Sci Rep

Ubiquitin C-terminal hydrolase L1 (UCHL1) regulates post-myocardial infarction cardiac fibrosis through glucose-regulated protein of 78 kDa (GRP78). [Abstract]

2020 Jun 30;10(1):10604. PMID: 32606430
Cancers (Basel)

Integrin α6β4 Upregulates PTPRZ1 Through UCHL1-Mediated Hif-1α Nuclear Accumulation to Promote Triple-Negative Breast Cancer Cell Invasive Properties. [Abstract]

2024 Oct 31;16(21):3683. PMID: 39518121
FASEB J

Cullin 2-RBX1 E3 ligase and USP2 regulate antithrombin ubiquitination and stability. [Abstract]

2021 Aug;35(8):e21800. PMID: 34324733
Anim Cells Syst

Blocking SLC7A11 attenuates the proliferation of esophageal squamous cell carcinoma cells. [Abstract]

2024 May 11;28(1):237-250. PMID: 38741950
Mol Oral Microbiol

UCHL1 Exacerbates Periodontitis by Coordinating Mitochondrial Dysfunction and Endoplasmic Reticulum Stress in Macrophages. [Abstract]

2026 Aug;41(4):201-215. PMID: 41919688
Exp Dermatol

Inhibition of Ubiquitin C-Terminal Hydrolase L1 Facilitates Cutaneous Wound Healing via Activating TGF-β/Smad Signalling Pathway in Fibroblasts. [Abstract]

2024 Oct;33(10):e15186. PMID: 39367569
Biochem Biophys Res Commun

Ubiquitin C-Terminal Hydrolase L1 regulates autophagy by inhibiting autophagosome formation through its deubiquitinating enzyme activity. [Abstract]

2018 Mar 4;497(2):726-733. PMID: 29462615

LDN-57444 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Mar 4;497(2):726-733. [Abstract]

Drug screen of UCHL1 and the function of inhibitors in autophagy. Both LDN and NSC could inhibit UCHL1 hydrolase activity. mRFP-GFP-LC3 stable cell line is treated with 5 μM LDN or 10 μM NSC in the condition of DMSO or Torin1 respectively for 6 h. The number of LC3 puncta remarkably is raised both in LDN and NSC treatment cells compared to the control.

LDN-57444 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Mar 4;497(2):726-733. [Abstract]

Drug screen of UCHL1 and the function of inhibitors in autophagy. Both LDN and NSC could inhibit UCHL1 hydrolase activity. Each cell lysate is analyzed by immunoblotting with anti p62 and LC3 antibodies.
J Surg Oncol

UCH-L1-containing exosomes mediate chemotherapeutic resistance transfer in breast cancer. [Abstract]

2017 Jun;115(8):932-940. PMID: 28334432

LDN-57444 purchased from MedChemExpress. Usage Cited in: J Surg Oncol. 2017 Jun;115(8):932-940. [Abstract]

p-ERK1/2 and ERK1/2 P-gp protein level are assessed by Western blot.
Int J Clin Exp Med

2016;9(8):15561-15567.
bioRxiv

2026 May 19.
Washington University

2025.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (62.87 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5148 mL

12.5742 mL

25.1484 mL

5 mM

0.5030 mL

2.5148 mL

5.0297 mL

10 mM

0.2515 mL

1.2574 mL

2.5148 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (25.15 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

To start an assay, 0.5 μL of 5 mg/mL test compound (including LDN-57444, about 50 μM final reaction concentration) or DMSO control is aliquoted into each well. Both enzyme and substrate are prepared in UCH reaction buffer (50 mM Tris-HCl [pH 7.6], 0.5 mM EDTA, 5 mM DTT, and 0.5 mg/mL ovalbumin). 25 μL of 0.6 nM UCH-L1 is then added to each well except substrate control wells, followed by plate shaking for 45-60 s on an automatic shaker. The enzyme/compound mixture is incubated at room temperature for 30 min before 25 μL of 200 nM Ub-AMC is added to initiate the enzyme reaction. The reaction mixture (300 pM UCH-L1, 100 nM Ubiquitin-AMC with 2.5 μg test compound) is incubated at room temperature for 30 additional minutes prior to quenching the reaction by the addition of 10 μL 500 mM acetic acid per well. The fluorescence emission intensity is measured on a LJL Analyst using a coumarin filter set (ex = 365 nm, em = 450 nm) and is subtracted by the intrinsic compound fluorescence to reveal the enzyme activity. A DMSO control (0.5 μL of DMSO, 25 μL of UCH-L1, 25 μL of ubiquitin-AMC, 10 μL of acetic acid), enzyme control (25 μL of UCH-L1, 25 μL of buffer, 10 μL of acetic acid), substrate control (25 μL of buffer, 25 μL of ubiquitin-AMC, 10 μL of acetic acid), and inhibitor control (0.5 μL of ubiquitin aldehyde [100 nM stock], 25 μL of UCH-L1, 25 μL of ubiquitin-AMC, 10 μL of acetic acid) are also performed in each assay plate to ensure quality and reproducibility. The UCH-L1 enzymatic reactions are manually repeated twice using the same protocol to confirm the results for the hit compounds from the primary robot-assisted screen^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[3]

Cell viability is measured by a quantitative colorimetric assay with MTT. After drug treatment SK-N-SH cells are incubated for 4 h with 5 g/L MTT and then DMSO is added for 15 min. The absorption is quantified at 570 nm using a micro-plate reader^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Each animal is placed individually into the conditioning chamber. The electric current is gradually increased (0.1 mA for 1 sec. at 30 sec. intervals increasing the shock intensity by 0.1 mA to 0.7 mA). Animal behavior is evaluated for the first visible response to the shock (flinch), the first extreme motor response (run/jump), and the first vocalized distress (scream). Threshold to flinching, jumping, and screaming is quantified for each animal by averaging of the shock intensity at which each animal manifests a behavioral response of that type to the foot shock. Visual, motor, and motivation skills are also tested with visible platform training by measuring the time and the speed to reach a visible platform placed within a pool filled with water. Both time to reach the platform and swimming speed are recorded and analyzed with a video tracking system. No difference is observed among different groups of mice in the experiments in which fear conditioning is tested both in the presence of LDN-57444 (LDN) and TAT fusion proteins. To decide the time of administration of LDN-57444, a series of preliminary experiments are performed in which the inhibitor is injected intra-peritoneally at different intervals (4 hrs before, 1 hr before, 1 hr after and 4 hrs after) from the electric shock. During the training phase, there is no difference in the freezing of LDN-57444- or vehicle-injected mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (459 KB)
- English - EN (459 KB)
- Français - FR (459 KB)
- Deutsch - DE (459 KB)
- Norwegian - NO (459 KB)
- Español - ES (459 KB)
- Swedish - SV (459 KB)
- Italian - IT (459 KB)
- Korean - KR (459 KB)
- Portuguese - PT (459 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Liu Y, et al. Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell line. Chem Biol. 2003 Sep;10(9):837-46. [Content Brief]

[2]. Gong B, et al. Ubiquitin hydrolase Uch-L1 rescues beta-amyloid-induced decreases in synaptic function and contextual memory. Cell. 2006 Aug 25;126(4):775-88. [Content Brief]

[3]. Tan YY, et al. Endoplasmic reticulum stress contributes to the cell death induced by UCH-L1 inhibitor. Mol Cell Biochem. 2008 Nov;318(1-2):109-15. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5148 mL	12.5742 mL	25.1484 mL	62.8709 mL
	5 mM	0.5030 mL	2.5148 mL	5.0297 mL	12.5742 mL
	10 mM	0.2515 mL	1.2574 mL	2.5148 mL	6.2871 mL
	15 mM	0.1677 mL	0.8383 mL	1.6766 mL	4.1914 mL
	20 mM	0.1257 mL	0.6287 mL	1.2574 mL	3.1435 mL
	25 mM	0.1006 mL	0.5030 mL	1.0059 mL	2.5148 mL
	30 mM	0.0838 mL	0.4191 mL	0.8383 mL	2.0957 mL
	40 mM	0.0629 mL	0.3144 mL	0.6287 mL	1.5718 mL
	50 mM	0.0503 mL	0.2515 mL	0.5030 mL	1.2574 mL
	60 mM	0.0419 mL	0.2096 mL	0.4191 mL	1.0478 mL

Keywords

LDN-57444

20 Cited Publications

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LDN-57444

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Ubiquitination Compound Library

Endoplasmic Reticulum Stress Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) LDN-57444

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LDN-57444

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Ubiquitination Compound Library

Endoplasmic Reticulum Stress Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) LDN-57444

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LDN-57444 Related Classifications

HY-18637 Related Classifications